Solubilization of poorly water-soluble compounds using amphiphilic phospholipid polymers with different molecular architectures

Mingwei Mu, Tomohiro Konno, Yuuki Inoue, Kazuhiko Ishihara

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)

Abstract

To achieve stable and effective solubilization of poorly water-soluble bioactive compounds, water-soluble and amphiphilic polymers composed of hydrophilic 2-methacryloyloxyethyl phosphorylcholine (MPC) units and hydrophobic n-butyl methacrylate (BMA) units were prepared. MPC polymers having different molecular architectures, such as random-type monomer unit sequences and block-type sequences, formed polymer aggregates when they were dissolved in aqueous media. The structure of the random-type polymer aggregate was loose and flexible. On the other hand, the block-type polymer formed polymeric micelles, which were composed of very stable hydrophobic poly(BMA) cores and hydrophilic poly(MPC) shells. The solubilization of a poorly water-soluble bioactive compound, paclitaxel (PTX), in the polymer aggregates was observed, however, solubilizing efficiency and stability were strongly depended on the polymer architecture; in other words, PTX stayed in the poly(BMA) core of the polymer micelle formed by the block-type polymer even when plasma protein was present in the aqueous medium. On the other hand, when the random-type polymer was used, PTX was transferred from the polymer aggregate to the protein. We conclude that water-soluble and amphiphilic MPC polymers are good candidates as solubilizers for poorly water-soluble bioactive compounds.

Original languageEnglish
Pages (from-to)249-256
Number of pages8
JournalColloids and Surfaces B: Biointerfaces
Volume158
DOIs
Publication statusPublished - 2017 Oct 1
Externally publishedYes

Keywords

  • MPC polymer
  • Paclitaxel
  • Polymer aggregate
  • Polymeric micelle
  • Solubilization
  • Water-soluble amphiphilic polymer

ASJC Scopus subject areas

  • Biotechnology
  • Surfaces and Interfaces
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry

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